Sphingosine 1-phosphate receptor 1, Sphingosine 1-phosphate receptor 3, Sphingosine 1-phosphate receptor 4, Sphingosine 1-phosphate receptor 5 (S1P1, S1P3, S1P4, S1P5)

Sphingosine 1-phosphate receptors (S1P1, S1P3, S1P4, S1P5) are G protein-coupled receptors that bind the bioactive lipid sphingosine 1-phosphate (S1P). These receptors mediate diverse biological functions including lymphocyte trafficking, vascular tone regulation, cardiac function, as well as central nervous system processes. They are considered important therapeutic targets, especially for the treatment of autoimmune diseases such as multiple sclerosis, due to their role in regulating lymphocyte egress from lymphoid tissues. Drugs targeting these receptors (notably S1P1 modulators) act primarily by promoting receptor internalization and thus retention of lymphocytes in nodes, modulating immunity with characteristic safety considerations such as transient bradycardia and increased infection risk[1][2][3][5][6].

Other names

S1PR1S1PR3S1PR4S1PR5EDG1 (S1P1)EDG3 (S1P3)EDG6 (S1P4)EDG8 (S1P5)

Agonists: internalization and functional antagonism of S1P receptors, resulting in sequestration of lymphocytes in lymph nodes, thus limiting egress into the circulation Modulation of downstream signaling pathways including Gi protein coupling, inhibition of adenylyl cyclase, ERK/MAPK activation